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US 5,632,969 AGranted
N.sub.3 S.sub.2 chelating ligands optionally radiolabelled with Tc or Re, useful for diagnostic or therapeutic applications
AssigneeMerck & Co., Inc.
InventorsRichard J. Flanagan, Jean-Marc Dufour, Keith T. Hogan
Life of this patent
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Abstract
Novel N.sub.3 S.sub.2 chelating ligands can be chelated to a radiodetectable element, Tc or Re, and are useful for radiolabeling peptides. A group of peptides especially useful are somatostatin derivatives which are valuable of the selective detection or treatment of tumors with somatostatin receptors.
Claims10
A compound of the formula:
- ##STR4## wherein:
- R is selected from the group consisting of:
- hydrogen,
- loweralkyl of 1-4 carbon atoms, and
- loweralkyl carboxyl, wherein loweralkyl is 1-4 carbon atoms;
- R.sup.1 is selected from the group consisting of:
- hydrogen, a sulfur protecting group, or where the two R.sup.1 groups are replaced by a disulfide linkage;
- R.sup.2 is selected from the group consisting of:
- ##STR5## n and m are independently an integer from 1-4;
- with the proviso that if R.sup.2 is -N=C=S or -NH.sub.2, and R is hydrogen or loweralkyl carboxyl, then the two R.sup.1 groups are replaced by a disulfide linkage.
7 more elements
A compound of the formula:
- ##STR6## wherein:
- R is hydrogen;
- the two R.sup.1 groups are replaced by a disulfide linkage;
- R.sup.2 is:
- ##STR7## and n is 2.
2 more elements
A compound of the formula:
- ##STR8## wherein:
- R is CH.sub.3 ;
- R.sup.1 is p-methoxybenzyl;
- R.sup.2 is:
- ##STR9## and n is 1.
2 more elements
A compound which is:
- 4-isothiocyanato-N-[2-(3,3,5,11,13,13-hexamethyl-1,2-dithia-5,8,11-triazacy clotridecan-8-yl)ethyl]benzamide.
Dependencies are inferred from the claim text.